Assay Detail
Binding
CHEMBL4322161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Potassium channel subfamily K member 9 (CHEMBL2321614) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
TASK Channels Pharmacology: New Challenges in Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 4.29 | 4.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1534525 | MIBEFRADIL DIHYDROCHLORIDE | 4.0 | 1 | 4.61 |
| CHEMBL1256755 | — | — | 1 | 4.34 |
| CHEMBL3039432 | — | — | 1 | 4.32 |
| CHEMBL30432 | GW282974X | — | 1 | 4.30 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 4.20 |
| CHEMBL1256660 | — | — | 1 | 4.13 |
| CHEMBL64249 | CLOROTEPINE | 2.0 | 1 | 4.13 |
| CHEMBL4458347 | — | — | 1 | - |
| CHEMBL54440 | MEVASTATIN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1534525 | MIBEFRADIL DIHYDROCHLORIDE | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL1256755 | — | IC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL3039432 | — | IC50 | = | 47700.0 | nM | 4.32 |
| CHEMBL30432 | GW282974X | IC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL998 | LORATADINE | IC50 | = | 63400.0 | nM | 4.20 |
| CHEMBL1256660 | — | IC50 | = | 73800.0 | nM | 4.13 |
| CHEMBL64249 | CLOROTEPINE | IC50 | = | 73800.0 | nM | 4.13 |
| CHEMBL4458347 | — | IC50 | = | 73.8 | % | - |
| CHEMBL54440 | MEVASTATIN | IC50 | = | 159000.0 | nM | - |